Home Tools
Log in
Cart

T-5224

Catalog No. T5416   CAS 530141-72-1

T-5224 is a transcription factor c-Fos/AP-1 inhibitor, which specifically inhibits the DNA binding activity of c-Fos/c-Jun without affecting other transcription factors.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
T-5224 Chemical Structure
T-5224, CAS 530141-72-1
Pack Size Availability Price/USD Quantity
1 mg In stock $ 41.00
2 mg In stock $ 59.00
5 mg In stock $ 97.00
10 mg In stock $ 147.00
25 mg In stock $ 267.00
50 mg In stock $ 447.00
100 mg In stock $ 659.00
500 mg In stock $ 2,150.00
1 mL * 10 mM (in DMSO) In stock $ 109.00
Bulk Inquiry
Get quote
Select Batch  
Purity: 99.29%
Purity: 98.01%
Contact us for more batch information
Biological Description
Chemical Properties
Storage & Solubility Information
Description T-5224 is a transcription factor c-Fos/AP-1 inhibitor, which specifically inhibits the DNA binding activity of c-Fos/c-Jun without affecting other transcription factors.
In vitro In vitro production of the synovial cell mediators MMP-1, MMP-3, IL-6 and TNFα by IL-1b–stimulated human synovial SW982 cells was inhibited by T-5224. This was also the case for the chondrocyte inflammatory mediators MMP-3 and MMP-13 in IL-1b–stimulated human chondrocyte SW1353 cells. The IC50 values were ~10 μM for most of the cellular assays [1]. Vasopressin selectively stimulates an increase CDS1 mRNA that is dependent on protein kinase C and can be inhibited by the AP-1 inhibitor, T-5224 [3]. T-5224 significantly inhibited the invasion, migration, and MMP activity of HNSCC cells in a dose-dependent manner; there was no significant influence on cell proliferation [4].
In vivo T-5224 efficiently inhibited the development of collagen-induced arthritis (CIA) when administered once daily from day 21, before the onset of arthritis. Arthritis on day 50 was inhibited by 64% and 91%, by 3 and 30 mg/kg of T-5224, respectively. The body weight of mice treated with T-5224 steadily recovered. X-ray studies showed that joint destruction was inhibited in treated but not in untreated arthritis controls, and notably, the joint was totally protected from destruction by 30 mg/kg of T-5224 [1]. Administration of T-5224 (300 mg/kg, p.o.) after intraperitoneal injection of LPS imparted appreciable protection against acute elevations in serum levels of TNFα, HMGB1, ALT/AST as well as in liver tissue levels of MIP-1α and MCP-1, and reduced the lethality (27 %) [2]. T-5224 (150 mg/kg) or vehicle was given orally every day for 4 weeks. The rate of cervical lymph node metastasis in the model was 40.0% in the T-5224-treated group versus 74.1% in the vehicle-treated group [4].
Kinase Assay The DNA binding activity of transcription factors was measured using the TransAM kits. Nuclear extracts containing factors such as c-Fos/AP-1, c-Jun/AP-1, ATF-2, C/EBPa, MyoD, Sp-1 or NF-kB/p65 and various concentrations of T-5224 were added in the multi-well plates precoated with respective consensus double-stranded (ds)DNA oligomers. After incubation for 1 h, the transcription factor bound to its respective consensus dsDNA sequences was detected by using antibodies reactive against the respective transcription factors according to the manufacturer's protocol [1].
Cell Research NIH/3T3 cells were transiently transfected with the luciferase reporter plasmids pAP-1-Luc (× 7 TGACTAA), pNF-kB-Luc (× 5 TGGGGACTTTCCGC) or control phRL-TK, and cultured overnight. Cells were incubated in 0.5% FBS/DMEM containing T-5224 for 1 h, and then stimulated with PMA (10 ng/ml) or TNFa (10 ng/ml), and then cultured for 3 h, followed by measurement of lysate by using dual-luciferase reporter assay system [1].
Animal Research Mice were housed in an SPF (specific pathogen-free) grade environment and provided food and water ad libitum with a 12 h:12 h light/dark cycle. Male 8-week-old DBA/1J mice were immunized with bovine type II collagen emulsified in Freund's complete adjuvant on days 0 and 21. T-5224, MTX and LEF were orally administered once per day. Arthritis was assessed in a blind fashion for four paws per mouse using the following score: 0, uninvolved; 1, swelling of ≤2 toes or slight swelling in ankles and wrists; 2, swelling of ≥3 toes or moderate swelling in ankles and wrists; 3, extensive swelling of total paw. X-ray films of four paws taken using Softex were assessed for joint destruction in 2nd to 5th proximal interphalangeal joints and five metatarsophalangeal joints of four paws, the carpal joints of the forepaws, and the tarsal and calcaneal joints of the hind paws. Score was: 0, no change; 1, partial erosion; 2, complete erosion for joints; and 0, negative; 0.5, positive for osteoporosis. IL-1β (500 ng per unilateral hind paw) was administered into the footpads. The mice with ≥1 arthritis score were treated with either anti-TNFα antibody at 50 or 250 μg/mouse, intraperitoneally (i.p.) twice a week and/or with 3 mg/kg T-5224, orally once daily [1].
Molecular Weight 517.53
Formula C29H27NO8
CAS No. 530141-72-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: Insoluble

DMSO: 50 mg/mL (96.61 mM)

TargetMolReferences and Literature

1. Aikawa Y, et al. Treatment of arthritis with a selective inhibitor of c-Fos/activator protein-1. Nat Biotechnol. 2008 Jul;26(7):817-23. 2. Izuta S, et al. T-5224, a selective inhibitor of c-Fos/activator protein-1, attenuates lipopolysaccharide-induced liver injury in mice. Biotechnol Lett. 2012 Dec;34(12):2175-82. 3. Blunsom NJ, et al. Sustained phospholipase C stimulation of H9c2 cardiomyoblasts by vasopressin induces an increase in CDP-diacylglycerol synthase 1 (CDS1) through protein kinase C and cFos. Biochim Biophys Acta Mol Cell Biol Lipids. 2019 Jul;1864(7):1072-1082. 4. Kamide D, et al. Selective activator protein-1 inhibitor T-5224 prevents lymph node metastasis in an oral cancer model. Cancer Sci. 2016 May;107(5):666-73.

TargetMolCitations

1. Wang X, Li K, Cheng M, et al.RNPS1 stabilizes NAT10 protein to facilitate translation in cancer via tRNA ac4C modification.bioRxiv.2023: 2023.02. 11.528122.

Related compound libraries

This product is contained In the following compound libraries:
Anti-COVID-19 Compound Library NO PAINS Compound Library ReFRAME Related Library Bioactive Compounds Library Max Transcription Factor-Targeted Compound Library Bioactive Compound Library Anti-Fibrosis Compound Library Inhibitor Library Protease Inhibitor Library Angiogenesis related Compound Library

Related Products

Related compounds with same targets
Auraptene Batimastat sodium salt MMP-7-IN-2 Lucidenic acid C FN-439 TFA Triolein Doxycycline hydrochloride CGS 27023A

TargetMolDose Conversion

You can also refer to dose conversion for different animals. More

TargetMol In vivo Formulation Calculator (Clear solution)

Step One: Enter information below
Dosage
mg/kg
Average weight of animals
g
Dosing volume per animal
ul
Number of animals
Step Two: Enter the in vivo formulation
% DMSO
%
% Tween 80
% ddH2O
Calculate Reset

TargetMolCalculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculation
Molecular Weight Calculator
=
X
X

Molarity Calculator allows you to calculate the

  • Mass of a compound required to prepare a solution of known volume and concentration
  • Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Concentration of a solution resulting from a known mass of compound in a specific volume
See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

X
=
X

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

=
/

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

T-5224 530141-72-1 Proteases/Proteasome MMP Activator Protein 1 Inhibitor inhibit Matrix metalloproteinases T 5224 AP-1 T5224 inhibitor

 

TargetMol